This invention relates to analgesics, specifically to a method of controlling inflammation and pain.
All early attempts at controlling pain were eventually superseded. Shortcomings of effectiveness and negative side effects were the reasons. This has been true since the historic use of herbs. Until 1955 aspirin was the primary over the counter inflammation and pain drug. It relieves inflammation and pain, but is particularly antagonistic to the stomach. Long term use may cause bleeding and ulcers.
Acetaminophen was introduced as an analgesic without the side effects of aspirin. However, it has no effect on inflammation and it can only be used as an analgesic. Although acetaminophen does not distress the stomach, continued use will tax the liver.
Other pharmaceuticals aimed at controlling inflammation and pain are continually introduced. The broadest category is known as NSAID (Non-Steroid Anti-Inflammatory Drug).
In the case of ADVIL (the trademark name of the drug ibuprofen), both inflammation and pain can be controlled. However, ADVIL (i.e. ibuprofen) has has serious side effects, being harmful to the stomach, kidneys or liver. It also causes ringing in the ears and dizziness.
ORUDIS (the tradmark name of the drup ketaprofen), an anti-inflammatory, has the same side effects as ibuprofen. In addition, it has particular cautions for patients with ulcers or kidney disease.
ALEVE (the trademark name for the drug naproxen sodium), is an anti-inflammatory but must not be taken by patients with kidney disease or liver impairment. Also, it may cause stomach ulcers.
INDOCIN (the trademark name for the drug indomethacin), is an anti-inflammatory broadly prescribed for arthritis. However, it has no more effect on arthritis than a placebo (as reported by the American Rheumatism Association). Its side effects, among many, include liver damage and hemorrhage of the esophagus.
The newest generation of NSAIDs are COX2 inhibitors. These are widely used prescription only drugs for inflammation and pain. They are considered a more effective class of NSAID. However, as historically demonstrated, they too have a lengthy list of side effects and precautions. CELEBREX (the trademark name of the drug celecoxib) and VIOXX (the trademark drug rofecoxib) comprise the main source of COX2 inhibitors.
The following is from the patient prescription information included with a CELEBREX prescription provided by CVS, a nationwide drugstore.
xe2x80x9cUSES: This medication is a non-steroidal anti-inflammatory drug (NSAID) which relieves pain and inflammation (swelling). It is used to treat pain, swelling and stiffness due to arthritis.
SIDE EFFECTS: Stomach upset, diarrhea, gas or nausea may occur. If these effects persist or worsen, notify your doctor promptly. Unlikely but report:promptly black or bloody stools or persistent stomach pain. Very unlikely but report promptly: unusual fatigue, yellowing eyes or skin, severe headache, unexplained weight gain or change in amount of urine. In the unlikely event you have an allergic reaction to this drug, seek immediate medical attention. Symptoms of an allergic reaction include rash, itching, swelling, dizziness or trouble breathing. If you notice other effects not listed above, contact your doctor or pharmacist.
PRECAUTIONS: Tell your doctor your medical history, including any allergies to drugs such as sulfas or asprin type drugs (NSAIDs); kidney, liver or heart disease; alcohol use, high blood pressure, swelling (edema), blood disorders (anemia), serious infections, stomach problems (bleeding or ulcers), asthma, or growths in the nose (nasal polyps). This medicine may cause stomach bleeding. Daily use of alcohol, especially when combined with this medicine, may increase your risk for stomach bleeding. Check with your doctor or pharmacist for more information. This medication should be used only when clearly needed during the first 3 months of pregnancy. It is not recommended for use during the last 6 months of pregnancy. Discuss the risks and benefits with your doctor. It is not known whether this drug is excreted into breast milk. Due to the potential risk to the infant, breast feeding while using this drug is not recommended. Consult your doctor before breast feeding. Caution is advised when this drug is used in the elderly, as they may be more sensitive to the side effects of this medication.
DRUG INTERACTIONS: Tell your doctor of all prescription and non-prescription drugs you may use, especially fluconazone, lithium, xe2x80x9cwater pillsxe2x80x9d (diuretics, e.g., furosemide, hydrochlorothiazide), drugs for high blood pressure, xe2x80x9cACE inhibitorsxe2x80x9d (e.g. captopril, lisinopril), xe2x80x9ccorticosteroidsxe2x80x9d (e.g., prednisone-like drugs), xe2x80x9cblood thinnersxe2x80x9d (e.g.warfarin) or NSAIDs (e.g., ibuprofen, naproxen). Check all nonprescription medicine labels carefully, since many contain pain relievers/fever reducers (NSAIDs/aspirin) which are similar to this drug. Aspirin as prescribed by your doctor for reasons such as heart attack or stroke prevention (i.e. non-arthritis doses) should be continued. Consult your pharmacist. Do not stop any medicine without doctor or pharmacist approval.xe2x80x9d
My invention, ACI (acetaminophen, choline and inositol), controls inflammation and/or pain due to sciatica, injury, trauma and arthritis. In contrast to all NSAIDs, it has no harmful side effects to either the liver or kidneys. There are no known side effects to the stomach such as ulcers or bleeding. It will not harm the esophagus. Choline and inositolare completely natural to the body and are readily absorbed.
Choline and inositol are highly effective lipotropic agents. They are readily transported to and absorbed by the liver. Lipotropic agents produce lecithin in the liver to protect against cirrhosis and fatty liver damage. The combined action of choline and inositol is ameliorating to the antagonistic effects of acetaminophen on the liver.
A method for alleviating pain and inflammation using a composition of acetaminophen, choline and inositol, which does not provide any of the distresses to the patient as do NSAIDs. My invention is a composition of acetaminophen, choline and inositol. It is used as a non-distressing anti-inflammatory.
The main embodiment is a compound of acetaminophen, choline and inositol in a constant ratio. The dosage is variable dependent upon the severity of condition of the patient.
The preferred embodiment is the compound in capsule or tablet form. The practical dose should be considered 33.33% by weight of acetaminophen; 33.33% by weight of choline; and 33.33% by weight of inositol.
Acetaminophen, an analgesic, works in the peripheral nervous system. It blocks pain impulses of trauma from going to the brain. Acetaminophen, unlike aspirin or any other conventional anti-inflammatory, does not have any effect on prostaglandins. Acetaminophen is the neutral ingredient of my invention as it relates to prostaglandins. It acts only as a broad spectrum analgesic.
Choline is a neurotransmitter and lipotropic agent. Choline along with inositol combine with methionine, an amino acid, which is omnipresent in the body. In the liver they form lecithin and are processed by enzymes into phosphytidal choline. The phosphytidal choline is transported by the blood into the brain, where it readily passes the brain blood barrier. In the brain the amino acid pyroglutamate breaks down phosphytidal choline into two neurotransmitters, specifically acetylcholine and inositol.
The brain releases the acetycholine directly into the peripheral nervous system. The nerves release the acetylcholine into all muscle receptor sites which relax all cell membranes. This makes muscles softer and more flexible, and as a result, gives the patient pain relief.
In summary, the acetylcholine is released from the brain and is transported into the peripheral nervous system. There it accelerates and amplifies the effects of acetaminophen.
Inositol is a phospholipid constituent of cell membranes. Inositol is a neurotransmitter and lipotropic agent. It regulates the functions of messenger molecules from the brain to the nervous system. It transports the movement of sodium, potassium and the electrolytes in the cells. Inositol is required for proper formation and function of cell membranes. It affects nerve transmissions and helps transport fats in the body.
The electro-chemical actions of inositol are not yet fully understood. It is speculated that inositol aids in trauma and injury by stabilizing the electrical charge in cell membranes.
Healthy cells maintain an electrical balance with a negative charge inside the cell and a positive charge on the outside. Any injury that disrupts this electrical balance will cause pain. It is believed that inositol aids in restoring electrical balance to cell membranes.
Choline and inositol are methyl donors which create sterols in the body. These sterols are precursors to prostaglandins. Prostaglandins are hormone-like substances which can be either pro-inflammatory or anti-inflammatory. Injury and trauma cause an imbalance of prostaglandins. My invention promotes a sustained release of the anti-inflammatory pro staglandins.
The invention is a new form of NSAID. It is a composition of acetaminophen, choline, and inositol (ACI).
All forms of inositol can be used in the invention. Myo-inositol is the form most bio-available to the body.
All forms of choline can be used in the invention. Phosphatidyl choline as it is found in soy should not be used because of potential allergic reactions. Choline chloride can also be used, but it has a laxative effect in high doses.
For optimum effectiveness, my invention is best utilized when choline bitartrate is combined with myo-inositol and acetaminophen. Acetaminophen is a long time used, well established analgesic.
All three ingredients-acetaminophen, choline bitartrate (or other form), and myo-inositol (or other form), act synergistically throughout the body for maximum, safe analgesic action with effective anti-inflammatory activity.